4-Hydroxymethyl-1, 6, 8-trimethylfuro [2, 3-h] quinolin-2 (1 H)-one Induces Mitochondrial Dysfunction and Apoptosis upon Its Intracellular Oxidation

…, G Dodoni, C Frezza, A Guiotto, V Barbieri…

Index: Chilin, Adriana; Dodoni, Giuliano; Frezza, Christian; Guiotto, Adriano; Barbieri, Vera; Di Lisa, Fabio; Canton, Marcella Journal of Medicinal Chemistry, 2005 , vol. 48, # 1 p. 192 - 199

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Citation Number: 23

Abstract

We investigated the mechanism of cell death induced by a furoquinolinone derivative, namely, 4-hydroxymethyl-1, 6, 8-trimethylfuro [2, 3-h] quinolin-2 (1 H)-one (HOFQ), in the dark. Mitochondrial depolarization was found to be a causative event in HOFQ-induced apoptosis that was blunted either by replacing the 4-hydroxymethyl group with a methyl one, or by 4-methylpyrazole, an inhibitor of alcohol dehydrogenase (ADH). In vitro enzymatic ...